Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Numidargistat dihydrochloride (CB-1158) is a highly potent and orally active chemical compound that effectively inhibits arginase. It exhibits IC50 values of 86 nM and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride contributes to immuno-oncology, making it a valuable agent in the field [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | 待询 | 10-14周 | ||
50 mg | 待询 | 10-14周 | ||
100 mg | 待询 | 10-14周 |
产品描述 | Numidargistat dihydrochloride (CB-1158) is a highly potent and orally active chemical compound that effectively inhibits arginase. It exhibits IC50 values of 86 nM and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride contributes to immuno-oncology, making it a valuable agent in the field [1]. |
体外活性 | Numidargistat dihydrochloride is a potent and orally-bioavailable inhibitor of arginase, with IC 50 s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC 50 s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC 50, 122 nM). Numidargistat dihydrochloride also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC 50 s of 32, 139, 210 μM, respectively. Numidargistat dihydrochloride shows no effect on NOS. In addition, Numidargistat dihydrochloride is not directly cytotoxic to murine cancer cell lines [1]. |
体内活性 | Numidargistat dihydrochloride (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat dihydrochloride in combination with PD-L1 blockade or LY 188011 inhibits tumor growth in mice bearing CT26 cancer cells [1]. |
分子量 | 360.04 |
分子式 | C11H24BCl2N3O5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Numidargistat dihydrochloride Inhibitor inhibitor inhibit